2374740-21-1

AKT-IN-3 (compound E22) is a potent, orally active low hERG blocking Akt inhibitor, with 1.4 nM, 1.2 nM and 1.7 nM for Akt1, Akt2 and Akt3, respectively. AKT-IN-3 (compound E22) also exhibits good inhibitory activity against other AGC family kinases, such as PKA, PKC, ROCK1, RSK1, P70S6K, and SGK. AKT-IN-3 (compound E22) induces apoptosis and inhibits metastasis of cancer cells[1].

Akt1: 1.4 nM (IC₅₀); Akt2: 1.2 nM (IC₅₀); Akt3: 1.7 nM (IC₅₀); PKA: 0.3 nM (IC₅₀); P70S6K: 8.9 (IC₅₀)

[1] Dong X, et al. Discovery of 3,4,6-Trisubstituted Piperidine Derivatives as Orally Active, Low hERG Blocking Akt Inhibitors via Conformational Restriction and Structure-Based Design. J Med Chem. 2019 Aug 8;62(15):7264-7288. DOI:10.1021/acs.jmedchem.9b00891